Galectin
Galectins are a subfamily of lectin proteins with high affinity for β-galactosides. In normal tissue and blood, galectins are expressed at low levels, but they are increased in serum, plasma and urine in neoplastic diseases. Galectins also play an important role in other chronic diseases such as cardiac insufficiency, diabetes, rheumatoid arthritis, asthma and liver cirrhosis. Galectins are present in numerous locations within the cell, such as nucleus, cytoplasm and plasma membrane, but also extracellularly. Gal-1 can recognize N-glycans on VEGFR2 and trigger a VEGF-like signaling response thereby promoting vascular regrowth in absence of VEGF. Galectins are involved in cancer-promoting processes such as proliferation, apoptosis and immune modulation. Galectins produced by tumor cells bind to T-cell glycoprotein receptors like CD45 and CD71. Potential adverse effects of galectin inhibition were observed in human breast carcinoma. In breast cancer cells, Gal-1 and Gal-3 compete for cell surface receptors while generating opposite functions. Gal-3 binds with K-Ras and activates the MEK-ERK signaling pathway, while Gal-1 binds with H-Ras and activates PI3K/AKT cascade hence modulating rather distinct cellular functions.
References
1.Kamil Wdowiak,et al. Int J Mol Sci. 2018 Jan; 19(1): 210.
References
1.Kamil Wdowiak,et al. Int J Mol Sci. 2018 Jan; 19(1): 210.
Cytoskeleton/Cell Adhesion Molecules
Galectin
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Thiodigalactoside
catalog no : M35002
cas no: 51555-87-4
Thiodigalactoside (TDG), a non-metabolizable disaccharide, serves as an orally active, potent galectin (GAL) inhibitor, exhibiting Kd values of 24 μM and 49 μM for GAL1 and GAL3, respectively. -
LLS30
catalog no : M13409
cas no: 2138367-58-3
LLS30 is a potent, allosteric Galectin-1 (Gal-1) inhibitor. -
GB1107
catalog no : M13093
cas no: 1978336-61-6
GB1107 (GB-1107, GB 1107) is a potent, selective, orally active inhibitor of Galectin-3 (Gal-3) with Kd of 37 nM (human Galectin-3). -
OTX008 (b)
catalog no : M12472
cas no: 1638140-55-2
OTX008 (Calixarene 0118, PTX-008) is a calixarene derivative designed to bind the Galectin-1 (Gal1) amphipathic β-sheet conformation. -
TD-139
catalog no : M11938
cas no: 1450824-22-2
TD-139 (TD139) is a highly potent, selecitve inhibitor of Galectin-3 (Gal-3) carbohydrate binding domain with Ki of 14 nM.